Adiposity (or excess fat in the subcutaneous cellular tissue) may have many causes, of varying complexity, and the understanding of which also varies greatly.
Some skin cells, known as adipocytes, contain variable amounts of fats in the form of triglycerides, which are synthesized in vivo via enzymatic reactions (lipogenesis), starting from free fatty acids and glycerol contained in the body and supplied to it via certain foods. Glycerol is obtained in vivo, by degradation of glucose. Now, in parallel, the triglycerides stored in the adipocyte cells may also be redegraded, under the action of specific lipolytic enzymes contained in these same cells. Redegradation liberates fatty acids, on the one hand, and glycerol and/or glycerol mono- and/or diesters, on the other hand. The fatty acids may then either diffuse in the body to be consumed or converted therein in different ways, or be taken up again (immediately or slightly later) by the adipocytes to again generate triglycerides by lipogenesis.
For various reasons (i.e. excessively rich food, inactivity, ageing and others), a substantial imbalance is established in the body between lipogenesis (i.e. the formation of triglycerides by enzymatic reaction between fatty acids and glycerol obtained from glucose) and lipolysis (i.e. the enzymatic decomposition of triglycerides into fatty acids and glycerol). Accordingly, if the amount of fatty substances formed by lipogenesis become appreciably and consistently greater than those which are eliminated by lipolysis, an accumulation of triglycerides occurs in the adipocytes. If this becomes excessive, it may be progressively reflected in the appearance of a thick skin with an often irregular surface ("orange-like skin") of a consistency which is flaccid or gelatinous to a greater or lesser extent. The final result is figure with an unattractive general appearance which may progress from the simple local excess (lipodismorphy), passing through a certain stoutness, and finally genuine obesity.
In view of the profound discomfort, both physical and aesthetic, and sometimes psychological, which it often causes in individuals suffering from it, in particular in women, adiposity nowadays constitutes a condition which is less and less well tolerated or accepted.
Methods have been proposed to treat adiposity, however, only the surgical methods, such as liposuction, currently provide truly satisfactory results. However, liposuction has the major drawback of being an invasive operation, which is intricate, not without risk and often expensive.
Accordingly, there is a strong need for a "mild" cosmetic and/or non-surgical therapeutic treatment which effectively combats against human or animal adiposity. In particular, there is a need to obtain a general or, on the contrary, localized effect of slimming and/or thinning of the skin or of the figure.
The present invention is aimed precisely at satisfying such a need.
Thus, after considerable research conducted in this matter analysis and interpretation of the multiple causes, factors and mechanisms, partly known per se, associated with adiposity, it has now been found, quite unexpectedly and surprisingly, that the above objective is achieved using a novel treatment process, which consists essentially of limiting, or in totally inhibiting the glucose uptake by the adipocyte cells, contained in the skin. Thus, by limiting or by preventing the diffusion of extracellular glucose into adipocytes (which "exhausts" the source of glycerol, essential for the storage of fats), it is possible to substantially decrease, the formation of the triglycerides in adipocytes which are normally generated by lipogenesis from the free fatty acids originating either from the diet or from lipolysis itself. It has been found that the desired technical effect could be obtained, by supplying the body, in particular the skin cells, with certain specific non-cytotoxic substances capable of effectively inhibiting glucose uptake by the adipocytes. Finally, it has been found that their effects can be further reinforced when glucose-uptake inhibitors are administered in conjunction with at least one compound capable of stimulating or activating lipolysis. Such a combination has been found to synergistically inhibit triglyceride formation.
All these discoveries form the basis of the present invention.